[EN] HETEROARYL-SUBSTITUTED TRIAZOLES AS APJ RECEPTOR AGONISTS [FR] TRIAZOLES SUBSTITUÉS PAR HÉTÉROARYLE UTILISÉS EN TANT QU'AGONISTES DU RÉCEPTEUR APJ
Heteroaryl-substituted triazoles as APJ receptor agonists
申请人:AMGEN INC.
公开号:US11046680B1
公开(公告)日:2021-06-29
Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
式(I)和式(II)化合物、其药学上可接受的盐、前述任何化合物的立体异构体或其混合物是 APJ 受体的激动剂,可用于治疗心血管疾病和其他疾病。式 I 和式 II 的化合物具有如下结构: 其中变量的定义在本文中提供。
EP1634874
申请人:——
公开号:——
公开(公告)日:——
Structure–activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists
A series of 5,5-dimethylthiohydantoin derivatives were synthesized and evaluated for androgen receptor pure antagonistic activities for the treatment of hormone refractory prostate cancer. CH4933468 (32d) with a sulfonamide side chain not only exhibited antagonistic activity with no agonistic activity in the reporter gene assay but also inhibited the growth of bicalutamide-resistant cell lines. This compound also inhibited tumor growth of the LNCaP xenograft in mice dose-dependently. (c) 2010 Elsevier Ltd. All rights reserved.
HETEROARYL-SUBSTITUTED TRIAZOLES AS APJ RECEPTOR AGONISTS
申请人:Amgen Inc.
公开号:EP3541805B1
公开(公告)日:2020-10-14
Novel Imidazolidine Derivatives
申请人:Tachibana Kazutaka
公开号:US20070249697A1
公开(公告)日:2007-10-25
The present invention provides a compound represented by formula (I):
wherein n is an integer selected from 1 to 20, Q is
A is cyano or the like; B is hydrogen, halogen, or the like; X
1
and X
2
are each independently selected from O and S; E is a C
1-4
alkyl group; and R
1
, R
2
, R
3
and R
4
are each independently selected from a hydrogen atom and a C
1
-C
6
alkyl group, and a drug, a pharmaceutical composition containing the compound, and the like.